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5-할로겐 치환 uracil 들의 4-Thiosugar Nucleosides의 합성 (제 1 보)
김정균,이억석,김창배,보벡크,윗슬러,Kim Jack C.,Lee Euk-suck,Kim Chang-bae,Bobek Miroslav,Whistlee Roy L. Korean Chemical Society 1975 대한화학회지 Vol.19 No.2
와 5-iodo-pyrimidine nucleoside 의 4'-thio 유도체들은 2,3,5-tri-O-aceytl-4-thio-D-ribofuranosyl chloride 와 5-halogeno-2,4-bis(trimethylsiloxy)pyrimidine의 chloromercury 유도체를 축합시킨후 보호작용기를 제거함으로써 합성하였다. 4'-Thio 유도체들의 생물학적 활성도는 예비시험에서는 이에 대응하는 4'-oxygen 유도체들과 큰 차이가 나지 않지만 4'-thio유도체가 비교적 더높은 활성을 가진다는 사실은 흥미로운 일이며 앞으로 생화학적인 고찰을 계속하는 것은 가치있는 일임을 보여주고 있다. The 4'-thio analogs of the 5-bromo-and 5-iodo-pyrimidine nucleosides were prepared by condensation of 2,3,5-tri-O-acetyl-4-thio-${\alpha},{\beta}$-D-ribofuranosyl chloride with the chloromercury derivatives of 5-halogeno-2,4-bis(trimethylsiloxy)pyrimidine, followed by the removal of the protecting groups. Although the biological activities of the 4'-thio derivatives are not greatly different from the corresponding 4'-oxygen analogs in this preliminary test, the fact that the 4'-thio analogs have comparableihigh activities, is of interest, and indicates the value of further biochemical examinations.
Preparation and Polymerization of Alkenylsilanes
김정균,최순규,박은미,정인경,Kim, Chung Kyun,Choi, Soon Kyu,Park, Eun Mi,Jung, In Kyung Korean Chemical Society 1997 대한화학회지 Vol.41 No.2
The silyltriflates$(Ph_{3-n}SiH(OTf)_n)$have been produced by the reaction of triphenylsilane and triflic acid$(CF_3SO_3H)$at low temperature. These highly reactive compounds are a valuable reagent for the synthesis of numerous new functional substituted silane derivatives. The reaction of silyltriflates with alkenyl- and alkynylmagnesium bromide as well as organolithium compounds gave new silanes$Ph_2SiHR(R=\;C(CPh,\;CH=CH_2,\;CH_2CH=CH_2,\; (CH_2)_2CH=CH_2,\;(CH_2)_3CH=CH_2)$in high yields. The hydrosilation of prepared alkenyl- and alkynylsilanesPh_2SiHR$in the presence of a platinum catalyst(Pt/C) at high temperature$(200{\circ}C)$gave carbosilane polymers$((Ph_2SiCH=CPh)_n$and$(Ph_2Si(CH_2)m)n;\;m=2∼4, n{\ge}10)$along with five- and six-membered silaalkane ring compounds derived from intramolecular hydrosilation reactions. All of the prepared compounds are confirmed by NMR, UV, IR and mass spectroscopy as well as elemental analysis. 실릴트리플레이트$(Ph_{3-n}SiH(OTf)_n))$는 낮은 온도에서 트리펜일실란과 트리플산$(CF_3SO_3H)$의 반응에 의해 형성되며 이러한 화합물은 새로운 기능성 실란 유도체의 제조에 이용되고 있다. 실릴트리플레이트와 알캔일-, 알킨일마그네슘 브롬아이드 그리고 유기리티움 화합물과의 반응에 의해 새로운 실란 화합물 Ph_2SiHR(R=C{\equiv}(CPh,\;CH=CH_2,\;CH_2CH=CH_2,\;(CH_2)_2CH=CH_2,\;(CH_2)_3CH=CH_2)$을 높은 수율로 얻었다. 합성된 알켄일-, 알킨일실란은 백금촉매 하에서 카보실란 고분자$((Ph_2Si(CH_2)m)n;\;m=2∼4,\;n\le10)$5~6환고리 화합물을 형성하였다. 모든 생성물들은 NMR, UV, IR, 질량분석, 그리고 원소분석법에 의해 확인되었다.
김정균,이억석,두렌보스,Jack C. Kim,Lee Euk-suk,Charles C. Chang,Norman J. Doorenbos Korean Chemical Society 1975 대한화학회지 Vol.19 No.3
The intermediate, 17${\alpha}$-methyl-4-aza-5${\alpha}$-androstan-17${\beta}$-ol(Ⅸ) required for the synthesis of 4-(${\beta}$-guanidinoethyl)-17${\alpha}$-methyl-4-aza-5${\alpha}$-androstan-17${\beta}$-ol(V) was obtained through a reaction of 17${\alpha}$-methyl-3,5-seco-4-norandrostan-17${\beta}$-ol-5-on-3-oic acid(VI) with ammonium hydroxide followed by two reductions(platinum dioxide with hydrogen and lithium aluminium hydride). Condensation of Ⅸ with chloroacetonitrile under anhydrous condition, followed by reduction of the nitrile with lithium aluminium hydride gave 4-(${\beta}$-aminoethyl)-17${\alpha}$-methyl-4-aza-5${\alpha}$-androstan-17${\beta}$-ol(XI). The reaction of XI with 2-methyl-2-thiopseudourea or 3,5-dimethylpyrazole-1-carboxamidine, or cyanamide provided the title compound, V. Relaxation of the nictitating membrane, in the absence of mydriasis, is considered to be evidence of adrenergic neurone blockade. Thus the test compound(V) resembles that of the classical adrenergic neurone blocking agents. 4-(${\beta}$-Guanidinoethyl)-17${\alpha}$-methyl-4-aza-5${\alpha}$-androstan-17${\beta}$-ol(V)을 합성하는데에 필요한 중간화합물인 17${\alpha}$-methyl-4-aza-5${\alpha}$-androstan-17${\beta}$-ol(IX)은 4단계를 거쳐 합성하였으며 IX을 chloroacetonitrile과 축합반응을 한후 $LiAlH_4$로서 환원하여 4-(${\beta}$-aminoethyl)-17${\alpha}$-methyl-4-aza-5${\alpha}$-androstan-17${\beta}$-ol(XI)을 얻었다. Tktle compound인 V은 3가지의 시약, 2-methyl-2-thiopseudourea,3,5-dimethylpyrazole-1-carboxamidine, cyanamide를 각각 XI와 반응시켜 좋은 수득률을 얻었다. 약리작용의 실험결과 V은 classical한 adrenergic neurone blocking agents와 유사하며 혈압강하제로서의 전망은 좋다고 예상된다.
김정균,조원제,보벡크,윗슬러,Jack C Kim,Won-Jei Cho,Miroslay Bobek,Roy L. Whistler Korean Chemical Society 1975 대한화학회지 Vol.19 No.6
Unusual pyrimidine nucleoside인 5-fluoro-4'-thiouridine과 5-Chloro-4'-thiouridine을 5-fluoro-와 5-chlorouracil의 2,4-bis(trimethylsilyl) 유도체들을 만든후, 축합반응하여 합성하였다. Leukemia 1210 cell과 Streptococcus faecium에 대한 기초 생물화학적인 예비시험에 의하면 5-fluoro-4'-thiouridine은 5-fluorouridine보다 억제효과가 월등하여 항암제로서의 전망여하는 앞으로의 임상 화학적인 결과로 구명될것 이라고 예상된다. The syntheses of anomeric mixtures of 1-(4-thio-${\alpha},{\beta}$-D-ribofuranosyl)-5-fluoro-and 5-chlorouracils from their corresponding bis(trimethylsilyl) derivatives of 5-halogenouracils and 2,3,5-tri-O-acetyl-4-thio-${\alpha},{\beta}$-D-ribofuranosyl chloride are described. Preliminary biochemical studies showed that in leukemia 1210 cells and Streptococcus faecium, the ${\beta}$-anomeric 5-chloro-4'-thionucleoside is not greatly different from the corresponding 4'-oxygen analog. However, the 5-fluoro-4'-thionucleoside showed a growth inhibitory effect more than that of the oxygen counterpart. The potential chemotherapeutic use of the analog is to warrant further study.
Beckmann Rearrangement of Ring A Steroidal Oxime Using the Carbon tetrachloride-triphenylphosphine
김정균,최순규,박원우,이용태,Kim Jack C.,Choi Soon-Kyu,Park Won-Woo,Lee Yong-Tae Korean Chemical Society 1979 대한화학회지 Vol.23 No.1
벡크만 자리옮김반응의 실험조건은 대부분이 센산 (HCl, $H_2SO_4$, $PCl_5$등)이나, 고온과 같은 격렬한 반응조건을 사용하므로 이러한 조건은 자주 전위보다는 케토옥심의 이성질화를 일으킨다. $5{\alpha}$-cholestan-3-one oxime의 벡크만 전위에 온화하고 중성의 조건인 사염화탄소와 트리페닐포스핀을 사용하여 3-aza-A-homo-5${\alpha}$-cholestan-4-one을 얻었다. 이러한 새롭고, 온화하며 쉽고 빠른 베그만 전위를 소개하고 이러한 방법을 고전적인 벡크만 전위 시약인 폴리인산을 사용한 방법과 비교하였다. The experimental procedures of Beckmann rearrangement mostly involve the use of vigorous conditions such as strongly acidic reagents (conc. HCl, $H_2SO_4$, $PCl_5$, etc.) or elevated temperatures, which frequently cause isomerization of ketooximes prior to rearrangement.We have effected the Beckmann rearrangement on $5{\alpha}$-cholestan-3-one oxime using the carbon tetrachloride-triphenylphosphine reagent under mild, neutral conditions to give 3-aza-A-homo-$5{\alpha}$-cholestan-4-one. This new, mild, facile and rapid general method of Beckmann rearrangement is presented, and compared with the classical (more conventional) Beckmann reagent of polyphosphoric acid.
천연한약재(목통, 삼릉, 치자) 추출물의 항산화효과 및 항균활성효과
김정균,강영미,엄광식,고영민,김태영 경상대학교 농업생명과학연구원 2003 농업생명과학연구 Vol.37 No.4
한약재로 많이 이용되고 있는 목통, 삼릉 및 치자의 항산화활성과 항균활성 정도를 검토하기 위해 한약재를 물, 70% methanol(MeOH) 및 100% MeOH로 추출한 후 각 추출물의 페놀화합물함량, 전자공여능, hydroxy radical 소거효과, reducing power 및 항균활성시험을 하였다. 그 결과 실험에 사용한 3가지 한약재 모두 항산화효과와 항균활성이 뛰어났으며, 특히 목통 70% MeOH 추출물이 그 효과가 가장 컸으며 다음이 100% MeOH, 물추출물 순이었다. Antioxidant activity and antimicrobial activity of medicinal plants extracts from 3 edible or medicinal plant were examined. The extracts from Akebia quinate Decaisne, Scirusfluviatilis A. Gray, Gardenia jasminoides for. grandiflora Makino showed comparatively strong antioxidative activity on test. Electron donatating abilities and hydroxy radical scavenging ablities of 70% methanol, 100% methanol extracts were higher than thoes of water extracts. Some extracts of medicinal plants showed antimicrobial effect, especially, the extracts showed antimicrobial effect in the 70% methanol higher than other extracts.